PD158780 manufacturers
- PD158780
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- $77.00 / 5mg
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2025-09-22
- CAS:171179-06-9
- Min. Order:
- Purity: 99.16%
- Supply Ability: 10g
- PD158780
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- $1.00 / 1KG
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2020-02-01
- CAS:171179-06-9
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 200kgs
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| | PD158780 Basic information |
| Product Name: | PD158780 | | Synonyms: | N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine;Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl- (Related Reference);Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl-;PD 158780 solution;InSolution? PD 158780;PD 158780 - CAS 171179-06-9 - Calbiochem;InSolution PD 158780 - CAS 171179-06-9 - Calbiochem;PD 158780; PD-158780 | | CAS: | 171179-06-9 | | MF: | C14H12BrN5 | | MW: | 330.18 | | EINECS: | | | Product Categories: | | | Mol File: | 171179-06-9.mol |  |
| | PD158780 Chemical Properties |
| Melting point | 174.0 to 178.0 °C | | Boiling point | 499.6±45.0 °C(Predicted) | | density | 1.611±0.06 g/cm3 (20 ºC 760 Torr) | | storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | | solubility | DMSO: ≥20mg/mL | | form | Yellow solid | | pka | 5.80±0.30(Predicted) | | color | yellow |
| Hazard Codes | Xn | | Risk Statements | 22 | | HS Code | 2912.49.2600 |
| | PD158780 Usage And Synthesis |
| Uses | PD 158780 is a potent tyrosine kinase inhibitor of the epidermal growth factor receptor and has been shown to delay substantial growth of tumors in vivo tumor models. | | Definition | ChEBI: PD158780 is a pyridopyrimidine that is pyrido[3,4-d]pyrimidine-4,6-diamine in which the amino groups at positions 4 and 6 are substituted by a m-bromophenyl group and a methyl group, respectively. It is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity [IC50 values of 0.008, 49 and 52 nM for EGFR, ErbB2 (HER2) and Erb4 (HER4)]. It does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells. It has a role as an antineoplastic agent and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a pyridopyrimidine, a secondary amino compound, a member of bromobenzenes, a diamine and an aromatic amine. | | General Description | A potent inhibitor of the EGFR tyrosine kinase activity (8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC50 =49 nM) and MDA-MB-453 (IC50 = 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells. | | Biological Activity | Potent inhibitor of ErbB receptor family tyrosine kinases (IC 50 values are 0.008, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively) that does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G 1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells. | | Biochem/physiol Actions | Cell permeable: yes | | Synthesis | Example 60: Synthesis of N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine
N-(3-Bromophenyl)-6-fluoro-pyrido[3,4-D]pyrimidin-4-amine (0.20 g, 0.63 mmol) was placed in a pressure vessel and an ethanol solution of methylamine was added and reacted at 100 °C. After completion of the reaction, purification was carried out by alumina column chromatography with the eluent dichloromethane/methanol (99:1, v/v) to afford the target product N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine (0.07 g, 34% yield).
1H NMR (DMSO) δ 9.69 (1H, s), 8.75 (1H, s), 8.41 (1H, s), 8.21 (1H, brs), 7.93 (1H, brd, J = 7.6 Hz), 7.41-7.28 (2H, m), 7.06 (1H, s), 6.82 (1H, q, J = 5.0 Hz), 4.95 ( 3H, d, J = 5.0 Hz). | | storage | Store at -20°C | | References | [1] Patent: US5654307, 1997, A |
| | PD158780 Preparation Products And Raw materials |
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